Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca influx.
性状
Solid
IC50 & Target[1][2]
PLA2
7 μM (IC50)
体外研究(In Vitro)
In RBL 2H3 and bone marrow-derived mast cells (BMMCs), Ca entry is critical for exocytosis. Bromoenol lactone inhibits exocytosis when stimulated using a Ca ionophore A23187, which passively transports Ca down a concentration gradient and also in permeabilised mast cells where Ca entry is no longer relevant. Moreover, Bromoenol lactone has only a minor effect on antigen- or thapsigargin-stimulated Ca signalling, both the release from internal stores and sustained elevation due to Ca influx.
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